Tho T, Kleinebudde P, Sande S A
Dept. of Pharmaceutics, School of Pharmacy, University of Oslo, Norway.
AAPS PharmSciTech. 2001 Dec 3;2(4):27. doi: 10.1208/pt020427.
The aim of this study was to improve the formation of spherical pectin pellets by investigating the effect of additive concentration in the granulation liquid on the shape and size of the products as well as by identifying an optimal additive concentration.
High-methoxylated, low-methoxylated, and amidated low-methoxylated pectin types were evaluated in combination with different concentrations of methanol, ethanol, citric acid, lactic acid, and calcium chloride. Pellets were prepared in a power-consumption-controlled twin-screw extruder, then spheronized and dried. The moisture content of the extrudate was determined, and the final products were characterized by image analysis and sieving analysis. A cloud point test was employed for the identification of an optimal additive concentration.
The concentration of additive in the granulation liquid affected the moisture content of the extrudate and the shape, size, and mechanical stability of the pectin pellets. Improvements in the pellet characteristics are dependent on the pectin type employed. The 2 low-methoxylated pectins were more sensitive to concentration changes than was the high-methoxylated type. Above a certain threshold concentration, the quality of the pellets are improved. This additive concentration differs according to type of pectin and type of additive.
It was demonstrated that there is a concentration-dependent interaction between pectin and substances added to the granulation liquid that can be utilized to improve the formation of spherical pectin pellets.
本研究的目的是通过研究制粒液中添加剂浓度对产品形状和尺寸的影响以及确定最佳添加剂浓度，来改善球形果胶微丸的成型。
对高甲氧基化、低甲氧基化和酰胺化低甲氧基化果胶类型与不同浓度的甲醇、乙醇、柠檬酸、乳酸和氯化钙进行组合评估。在功耗控制的双螺杆挤出机中制备微丸，然后进行滚圆和干燥。测定挤出物的水分含量，并用图像分析和筛分分析对最终产品进行表征。采用浊点试验确定最佳添加剂浓度。
制粒液中添加剂的浓度影响挤出物的水分含量以及果胶微丸的形状、尺寸和机械稳定性。微丸特性的改善取决于所使用的果胶类型。两种低甲氧基化果胶比高甲氧基化果胶对浓度变化更敏感。高于一定阈值浓度时，微丸质量得到改善。该添加剂浓度因果胶类型和添加剂类型而异。
结果表明，果胶与添加到制粒液中的物质之间存在浓度依赖性相互作用，可利用该相互作用改善球形果胶微丸的成型。
